Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease

European Journal of Medicinal Chemistry
2019.0

Abstract

Previous studies showed repurposed drugs Clofazimine and Benidipine had antichagasic activity in acute and chronic Trypanosoma cruzi (T. cruzi) infection models as monotherapies. This study evaluated combinations of these drugs with low-dose Benznidazole (BZ, first-choice treatment in Argentina) against intracellular T. cruzi amastigotes in vitro and in a chronic murine model. In vitro, both BZ+Clofazimine and BZ+Benidipine combinations exhibited additive/synergistic effects (synergy scores >0) across four reference models (Bliss, Loewe, HSA, ZIP) with no cytotoxicity to Vero cells. In vivo, all treatments reduced blood parasite burden (quantified by qPCR) vs. untreated controls, with Clofazimine+BZ 30 showing greater reduction than BZ 30 monotherapy. While tissue (skeletal/cardiac muscle) parasite burden differences were not statistically significant, trends toward reduction were observed. Combined therapies reduced inflammation (e.g., fewer adipocytes in skeletal muscle) compared to BZ alone, and low-dose BZ combinations avoided the body weight loss seen with high-dose BZ (75 mg/kg) monotherapy. These findings support that repurposed drugs combined with low-dose BZ could be alternatives for chronic Chagas disease, with synergistic in vitro interactions indicating adjusted dosing regimes can improve in vivo therapeutic efficacy.

Knowledge Graph

Similar Paper

Combined therapy with Benznidazole and repurposed drugs Clofazimine and Benidipine for chronic Chagas disease
European Journal of Medicinal Chemistry 2019.0
1,2,3-Triazole-based analogue of benznidazole displays remarkable activity against Trypanosoma cruzi
Bioorganic & Medicinal Chemistry 2015.0
In Vitro and in Vivo Anti-Trypanosoma cruzi Activity of New Arylamine Mannich Base-Type Derivatives
Journal of Medicinal Chemistry 2016.0
Second Generation of Mannich Base-Type Derivatives with in Vivo Activity against Trypanosoma cruzi
Journal of Medicinal Chemistry 2018.0
Candimine from Hippeastrum escoipense (Amaryllidaceae): Anti-Trypanosoma cruzi activity and synergistic effect with benznidazole
Phytomedicine 2023.0
Phthalimido-thiazoles as building blocks and their effects on the growth and morphology of Trypanosoma cruzi
European Journal of Medicinal Chemistry 2016.0
New polyamine drugs as more effective antichagas agents than benznidazole in both the acute and chronic phases
European Journal of Medicinal Chemistry 2019.0
In Vitro and in Vivo Trypanosomicidal Activity of Pyrazole-Containing Macrocyclic and Macrobicyclic Polyamines: Their Action on Acute and Chronic Phases of Chagas Disease
Journal of Medicinal Chemistry 2012.0
Complexation of the anti-Trypanosoma cruzi Drug Benznidazole Improves Solubility and Efficacy
Journal of Medicinal Chemistry 2008.0
Structural design, synthesis and pharmacological evaluation of thiazoles against Trypanosoma cruzi
European Journal of Medicinal Chemistry 2017.0